摘要
以邻氨基苯酚(硫酚)和尿素为起始原料,经一系列反应,合成出了30个新型含噁二唑环的苯并噁/噻唑啉酮衍生物(6).利用IR、1H NMR和元素分析对新化合物4和6的结构进行了表征.对所合成的目标化合物进行了抗癌、抗炎和免疫调节活性的筛选,实验结果表明,部分目标化合物具有弱的抗癌和免疫调节活性,对TNF-α和Cdc25B磷酸酯酶均无抑制活性.
Thirty novel benzoxazolinone/benzothiazolone derivatives（6） containing oxadiazole moiety were synthesized by 2-aminophenol or 2-aminothiophenol and urea as starting materials via a series of reac-tions.The structures of new intermediate 4 and the target compounds 6 were characterized by IR,1H NMR spectra and elemental analysis.The synthesized target compounds were screened for the anticancer,antiin-flammatory and immunoregulatory activities.The results indicated that some compounds exhibited weak ac-tivities in the anticancer and immunoregulatory fields,while all of them were found to be inactive against TNF-α and Cdc25B phosphatase.
出处
《化学学报》
SCIE
CAS
CSCD
北大核心
2012年第2期151-160,共10页
Acta Chimica Sinica
基金
辽宁省自然科学基金(No.20102126)资助项目~~
关键词
苯并噁/噻唑啉酮
噁二唑
合成
表征
生物活性
benzoxazolinone/benzothiazolone
oxadiazole
synthesis
characterization
bioactivity
